Title:
CDK9 INHIBITOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/109959
Kind Code:
A1
Abstract:
The present invention relates to the field of medicines, specifically relates to a CDK9 inhibitor compound represented by formula (I), and a pharmaceutically acceptable salt or isomer thereof, and also relates to a pharmaceutical composition and pharmaceutical preparation of the compound and a use thereof. X1, X2, R1, R2, R3, R6, A, L, n, and m are as defined in the description. The compound can be used in the preparation of a drug for treating or preventing CDK9-mediated related diseases.
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Inventors:
WU FRANK (CN)
LI LIN (CN)
WANG WUWEI (CN)
YOKOSAKA TAKUYA (JP)
MIYANO NATSUMI (JP)
KAWASAKI MASANORI (JP)
LI LIN (CN)
WANG WUWEI (CN)
YOKOSAKA TAKUYA (JP)
MIYANO NATSUMI (JP)
KAWASAKI MASANORI (JP)
Application Number:
PCT/CN2022/139704
Publication Date:
June 22, 2023
Filing Date:
December 16, 2022
Export Citation:
Assignee:
TRANSTHERA SCIENCES NANJING INC (CN)
TEIJIN PHARMA LTD (JP)
TEIJIN PHARMA LTD (JP)
International Classes:
C07D471/04; A61K31/4375; A61K31/439; A61K31/519; A61K31/5377; A61K31/5386; A61K31/55; A61P35/00; A61P35/02; C07D519/00
Domestic Patent References:
| WO2022037592A1 | 2022-02-24 | |||
| WO2021057853A1 | 2021-04-01 | |||
| WO2010094695A1 | 2010-08-26 |
Other References:
INNOCENTI, P. ET AL.: "Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds:synthesis and modification of pyrido[3,4-d]pyrimidines", ORG. BIOMOL. CHEM., vol. 13, no. 3, 19 November 2014 (2014-11-19), XP055332115, ISSN: 1477-0520, DOI: 10.1039/C4OB02238F
DATABASE Registry 3 May 2017 (2017-05-03), ANONYMOUS : "7-Isoquinolinamine, 1-c hloro-N-(1-methyl-4- piperidinyl)- (CA IND EX NAME)", XP093072821, retrieved from STN Database accession no. 2094907-55-6
DATABASE Registry 6 December 2015 (2015-12-06), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(phenyl methoxy)- (CA INDE X NAME)", XP093072822, retrieved from STN Database accession no. 1823295-18-6
DATABASE Registry 7 February 2014 (2014-02-07), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1,1-di methylethoxy)- (CA I NDEX NAME)", XP093072823, retrieved from STN Database accession no. 1538830-01-1
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "Ethanol, 2-[[7-(cycloprop ylamino)-1-isoquino linyl]methylamino]- (CA INDEX NAME)", XP093072824, retrieved from STN Database accession no. 1367738-48-4
DATABASE Registry 30 December 2013 (2013-12-30), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-ethoxy- (CA INDEX NAME)", XP093072826, retrieved from STN Database accession no. 1506804-51-8
DATABASE Registry 26 December 2013 (2013-12-26), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-metho xy- (CA INDEX NAM E)", XP093072827, retrieved from STN Database accession no. 1504100-94-0
DATABASE Registry 6 February 2014 (2014-02-06), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1-pipe razinyl)- (CA INDEX NAME) ", XP093072829, retrieved from STN Database accession no. 1538337-11-9
DATABASE Registry "L-Proline, 1-[7-(cyclopropylamino)-1-isoquinolinyl]-", XP093097519, retrieved from STN
DATABASE Registry 26 December 2023 (2023-12-26), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-(1,1-di methylethoxy)- (CA I NDEX NAME)", XP093072833, retrieved from STN Database accession no. 1369293-14-0
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1-pipe ridinyl)- (CA INDEX NAME)", XP093072841, retrieved from STN Database accession no. 1369286-27-0
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-(1-pipe razinyl)- (CA INDEX NAME)", XP093072842, retrieved from STN Database accession no. 1369282-72-3
DATABASE REGISTRY 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, 1- (1,1-dimethylethox y)-N-4-piperidinyl- (CA INDEX NAME)", XP093072844, retrieved from STN Database accession no. 1369280-17-0
DATABASE REGISTRY 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-metho xy- (CA INDEX NAM E) ", XP093072845, retrieved from STN Database accession no. 1369279-91-3
DATABASE REGISTRY 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(4-pipe ridinyloxy)- (CA IND EX NAME)", XP093072846, retrieved from STN Database accession no. 1369182-48-8
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-[(1-met hyl-4-piperidinyl)ox y]- (CA INDEX NAME)", XP093072955, retrieved from STN Database accession no. 1369182-34-2
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-[(1-met hyl-4-piperidinyl)ox y]- (CA INDEX NAME)", XP093072959, retrieved from STN Database accession no. 1369174-20-8
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1-pyrr olidinyl)- (CA INDEX NAME)", XP093072962, retrieved from STN Database accession no. 1368391-51-8
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "1,7-Isoquinolinediamin e, N7-cyclopentyl-N 1,N1-dimethyl- (CA I NDEX NAME)", XP093072967, retrieved from STN Database accession no. 1368254-30-1
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-4- piperidinyl-1-(3-pyri dinylmethoxy)- (CA I NDEX NAME)", XP093072970, retrieved from STN Database accession no. 1368088-62-3
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(4-mor pholinyl)- (CA INDEX NAME)", XP093072973, retrieved from STN Database accession no. 1368067-46-2
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, 1-m ethoxy-N-4-piperidi nyl- (CA INDEX NAM E)", XP093073008, retrieved from STN Database accession no. 1368062-17-2
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-[3-(dim ethylamino)propox y]- (CA INDEX NAME)", XP093073017, retrieved from STN Database accession no. 1368027-32-0
DATABASE REGISTRY 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, 1- [(1-methyl-4-piperid inyl)oxy]-N-4-piperid inyl- (CA INDEX NAME)", XP093073021, retrieved from STN Database accession no. 1367838-10-5
DATABASE REGISTRY 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, 1- [(1-methyl-4-piperid inyl)oxy]-N-4-piperid inyl- (CA INDEX NAME)", XP093073022, retrieved from STN Database accession no. 1367827-03-9
DATABASE REGISTRY 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-ethoxy- (CA INDEX NAME)", XP093073024, retrieved from STN Database accession no. 1367822-36-3
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, 1-(1 -methylethoxy)-N-4- piperidinyl- (CA IND EX NAME)", XP093073025, retrieved from STN Database accession no. 1367807-87-1
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(4-pipe ridinylmethoxy)- (CA INDEX NAME)", XP093073027, retrieved from STN Database accession no. 1367778-06-0
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "Glycine, N-[7-(cyclopent ylamino)-1-isoquino linyl]-N-methyl- (CA INDEX NAME)", XP093073029, retrieved from STN Database accession no. 1367744-99-7
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-[2-(dim ethylamino)ethoxy]- (CA INDEX NAME)", XP093073030, retrieved from STN Database accession no. 1367743-10-9
DATABASE Registry 22 December 2013 (2013-12-22), ANONYMOUS : "1,7-Isoquinolinediamin e, N7-cyclopropyl-N 1,N1-dimethyl- (CA I NDEX NAME)", XP093073031, retrieved from STN Database accession no. 1500319-19-6
DATABASE Registry 3 May 2017 (2017-05-03), ANONYMOUS : "7-Isoquinolinamine, 1-c hloro-N-(1-methyl-4- piperidinyl)- (CA IND EX NAME)", XP093072821, retrieved from STN Database accession no. 2094907-55-6
DATABASE Registry 6 December 2015 (2015-12-06), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(phenyl methoxy)- (CA INDE X NAME)", XP093072822, retrieved from STN Database accession no. 1823295-18-6
DATABASE Registry 7 February 2014 (2014-02-07), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1,1-di methylethoxy)- (CA I NDEX NAME)", XP093072823, retrieved from STN Database accession no. 1538830-01-1
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "Ethanol, 2-[[7-(cycloprop ylamino)-1-isoquino linyl]methylamino]- (CA INDEX NAME)", XP093072824, retrieved from STN Database accession no. 1367738-48-4
DATABASE Registry 30 December 2013 (2013-12-30), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-ethoxy- (CA INDEX NAME)", XP093072826, retrieved from STN Database accession no. 1506804-51-8
DATABASE Registry 26 December 2013 (2013-12-26), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-metho xy- (CA INDEX NAM E)", XP093072827, retrieved from STN Database accession no. 1504100-94-0
DATABASE Registry 6 February 2014 (2014-02-06), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1-pipe razinyl)- (CA INDEX NAME) ", XP093072829, retrieved from STN Database accession no. 1538337-11-9
DATABASE Registry "L-Proline, 1-[7-(cyclopropylamino)-1-isoquinolinyl]-", XP093097519, retrieved from STN
DATABASE Registry 26 December 2023 (2023-12-26), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-(1,1-di methylethoxy)- (CA I NDEX NAME)", XP093072833, retrieved from STN Database accession no. 1369293-14-0
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1-pipe ridinyl)- (CA INDEX NAME)", XP093072841, retrieved from STN Database accession no. 1369286-27-0
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-(1-pipe razinyl)- (CA INDEX NAME)", XP093072842, retrieved from STN Database accession no. 1369282-72-3
DATABASE REGISTRY 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, 1- (1,1-dimethylethox y)-N-4-piperidinyl- (CA INDEX NAME)", XP093072844, retrieved from STN Database accession no. 1369280-17-0
DATABASE REGISTRY 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-metho xy- (CA INDEX NAM E) ", XP093072845, retrieved from STN Database accession no. 1369279-91-3
DATABASE REGISTRY 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(4-pipe ridinyloxy)- (CA IND EX NAME)", XP093072846, retrieved from STN Database accession no. 1369182-48-8
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-[(1-met hyl-4-piperidinyl)ox y]- (CA INDEX NAME)", XP093072955, retrieved from STN Database accession no. 1369182-34-2
DATABASE Registry 16 April 2012 (2012-04-16), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-[(1-met hyl-4-piperidinyl)ox y]- (CA INDEX NAME)", XP093072959, retrieved from STN Database accession no. 1369174-20-8
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(1-pyrr olidinyl)- (CA INDEX NAME)", XP093072962, retrieved from STN Database accession no. 1368391-51-8
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "1,7-Isoquinolinediamin e, N7-cyclopentyl-N 1,N1-dimethyl- (CA I NDEX NAME)", XP093072967, retrieved from STN Database accession no. 1368254-30-1
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-4- piperidinyl-1-(3-pyri dinylmethoxy)- (CA I NDEX NAME)", XP093072970, retrieved from STN Database accession no. 1368088-62-3
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(4-mor pholinyl)- (CA INDEX NAME)", XP093072973, retrieved from STN Database accession no. 1368067-46-2
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, 1-m ethoxy-N-4-piperidi nyl- (CA INDEX NAM E)", XP093073008, retrieved from STN Database accession no. 1368062-17-2
DATABASE Registry 15 April 2012 (2012-04-15), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-[3-(dim ethylamino)propox y]- (CA INDEX NAME)", XP093073017, retrieved from STN Database accession no. 1368027-32-0
DATABASE REGISTRY 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, 1- [(1-methyl-4-piperid inyl)oxy]-N-4-piperid inyl- (CA INDEX NAME)", XP093073021, retrieved from STN Database accession no. 1367838-10-5
DATABASE REGISTRY 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, 1- [(1-methyl-4-piperid inyl)oxy]-N-4-piperid inyl- (CA INDEX NAME)", XP093073022, retrieved from STN Database accession no. 1367827-03-9
DATABASE REGISTRY 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-ethoxy- (CA INDEX NAME)", XP093073024, retrieved from STN Database accession no. 1367822-36-3
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, 1-(1 -methylethoxy)-N-4- piperidinyl- (CA IND EX NAME)", XP093073025, retrieved from STN Database accession no. 1367807-87-1
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, N-c yclopropyl-1-(4-pipe ridinylmethoxy)- (CA INDEX NAME)", XP093073027, retrieved from STN Database accession no. 1367778-06-0
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "Glycine, N-[7-(cyclopent ylamino)-1-isoquino linyl]-N-methyl- (CA INDEX NAME)", XP093073029, retrieved from STN Database accession no. 1367744-99-7
DATABASE Registry 13 April 2012 (2012-04-13), ANONYMOUS : "7-Isoquinolinamine, N-c yclopentyl-1-[2-(dim ethylamino)ethoxy]- (CA INDEX NAME)", XP093073030, retrieved from STN Database accession no. 1367743-10-9
DATABASE Registry 22 December 2013 (2013-12-22), ANONYMOUS : "1,7-Isoquinolinediamin e, N7-cyclopropyl-N 1,N1-dimethyl- (CA I NDEX NAME)", XP093073031, retrieved from STN Database accession no. 1500319-19-6
Attorney, Agent or Firm:
CHINA PATENT AGENT (H.K.) LTD. (CN)
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